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Scopolamine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Scopolamine图片
CAS NO:51-34-3

Hyoscine
Scopine (-)-tropate
Scopine tropate
Scopolamine 是高亲和力的 (nM 级别) 毒蕈碱 (muscarinic) 拮抗剂。Scopolamine 可逆抑制 5-HT3受体反应,IC50为 2.09 μM。
生物活性

Scopolamine is a high affinity (nM)muscarinicantagonist.5-HT3receptor-responses are reversibly inhibited by Scopolamine with anIC50of 2.09 μM.

IC50& Target

5-HT3Receptor

2.09 μM (IC50)

Human Endogenous Metabolite

 

mAChR

 

体外研究
(In Vitro)

Application of Scopolamine to oocytes expressing 5-HT3receptors does not elicit a response when applied alone, but causes a concentration-dependent inhibition of the response during a co-application of 2 μM 5-HT. The pIC50value for Scopolamine is 5.68±0.05 (IC50=2.09 μM, n=6) with a Hill Slope of 1.06 ± 0.05. This gave a Kbof 3.23 μM. The same concentration-dependent effect is also seen when Scopolamine is applied during the 5-HT application. To further test for a competitive binding at the 5-HT3receptor, the competition of unlabelled Scopolamine is measured with [3H]granisetron, an established high-affinity competitive antagonist at these receptors. Scopolamine displays concentration-dependent competition with 0.6 nM [3H]granisetron (~Kd), yielding an average pKiof 5.17±0.24 (Ki=6.76 μM, n=3)[1].

体内研究
(In Vivo)

In the histopathology study, there is no significant change in the histology of the brain. However, it is observed that there is a reduction in density of cells in the hippocampus of the control mice pretreated with Scopolamine who received only distilled water[2]. Scopolamine administration alone significantly increases the activity of Acetylcholinesterase enzyme (AchE) (7.98±0.065; P<0.001) when compared to the normal group (3.06±0.296). The animals treated with Scopolamine report a significant increase (34.61±4.85; P<0.01) in levels of malondialdehyde (MDA) as compared to the normal group (12.82±2.86). The Scopolamine-treated group shows significant decrease in reduced glutathione (GSH) level (P<0.001; 0.1504±0.03) as compared to the normal group (0.3906±0.02). The Scopolamine-treated rats show a significant increase in the concentration ofβ amyloid (Aβ1-42) (P<0.001; 146.2±1.74) as compared to the normal group (43.21±3.46)[3].

分子量

303.35

性状

Viscous liquid

Formula

C17H21NO4

CAS 号

51-34-3

中文名称

东莨菪碱

结构分类
  • Alkaloids
  • Other Alkaloids
来源
  • Plants
  • Solanaceae
  • Datura metelL.
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
In Vitro: 

DMSO : 100 mg/mL(329.65 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.2965 mL16.4826 mL32.9652 mL
5 mM0.6593 mL3.2965 mL6.5930 mL
10 mM0.3297 mL1.6483 mL3.2965 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.5 mg/mL (8.24 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.24 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.5 mg/mL (8.24 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.24 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (8.24 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.24 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。
 
 
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